ChEMBL ligand: CHEMBL4570444
stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Human [ChEMBL: CHEMBL4523377] [GtoPdb: 2902] [UniProtKB: Q86WV6] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523377] [GtoPdb: 2902] [UniProtKB: Q86WV6]
ChEMBL	STING Biochemical [3H]cGAMP Competition Assay: The individual compounds described in the Examples herein are defined as STING agonists by (i) binding to the STING protein as evidenced by a reduction in binding of tritiated cGAMP ligand to the STING protein by at least 20% at 20 uM (concentration of compound being tested) in a STING Biochemical 13H1-cGAMP Competition Assay and (ii) demonstrating interferon production with a 6% or greater induction of IFN-β secretion at 30 uM in the THP1 cell assay (where induction caused by cGAMP at 30 uM was set at 100%).The ability of compounds to bind STING is quantified by the ability to compete with tritiated cGAMP ligand for human STING receptor membrane using a radioactive filter-binding assay. The binding assay employs STING receptor obtained from Hi-Five cell membranes overexpressing full-length HAQ STING prepared in-house and tritiated cGAMP ligand also purified in-house.	B	5.41	pEC50	3873	nM	EC50	US-10730849-B2. Benzo[b]thiophene compounds as STING agonists (2020)
GtoPdb	Determined in a 3H-cGAMP filtration binding assay with hSTING protein	-	5.56	pEC50	2735	nM	EC50	US10730849B2. Benzo[b]thiophene compounds as STING agonists (2020)
ChEMBL	Displacement of [3H]-cGAMP from full length STING HAQ mutant in human THP1 cells by filtration binding assay	B	5.56	pEC50	2735	nM	EC50	J Med Chem (2020) 63: 3785-3816 [PMID:31820978]
ChEMBL	STING Biochemical [3H]cGAMP Competition Assay: The individual compounds described in the Examples herein are defined as STING agonists by (i) binding to the STING protein as evidenced by a reduction in binding of tritiated cGAMP ligand to the STING protein by at least 20% at 20 uM (concentration of compound being tested) in a STING Biochemical 13H1-cGAMP Competition Assay and (ii) demonstrating interferon production with a 6% or greater induction of IFN-β secretion at 30 uM in the THP1 cell assay (where induction caused by cGAMP at 30 uM was set at 100%).The ability of compounds to bind STING is quantified by the ability to compete with tritiated cGAMP ligand for human STING receptor membrane using a radioactive filter-binding assay. The binding assay employs STING receptor obtained from Hi-Five cell membranes overexpressing full-length HAQ STING prepared in-house and tritiated cGAMP ligand also purified in-house.	B	5.56	pEC50	2735	nM	EC50	US-10730849-B2. Benzo[b]thiophene compounds as STING agonists (2020)

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]